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    • 1. 发明授权
    • 세포수용체와HIV의상호작용을저해하는항AIDS펩타이드
    • 抑制细胞受体-HIV相互作用的抗艾滋病肽
    • KR100321275B1
    • 2002-05-13
    • KR1019980040708
    • 1998-09-30
    • 동화약품주식회사학교법인 포항공과대학교
    • 윤성준김종우성영철이경재신동혁김남두최요한박상진장환봉한진희
    • C07K7/08
    • 본 발명은 세포 수용체인 CD4와 인간 면역 결핍 바이러스-1 (human immunodeficiency virus type 1, 이하 "HIV-1"로 약칭함)의 외막 단백질인 gp120과의 상호작용을 저해하는 펩타이드, 그의 용도 및 이 펩타이드의 선별방법에 관한 것으로, 구체적으로는 12개의 아미노산으로 이루어지고 아미노 말단으로부터 4번 아미노산은 프롤린 (proline), 6번 아미노산은 페닐알라닌 (phenylalanine)이고 나머지는 임의의 아미노산인 펩타이드로서 세포 수용체인 CD4와 HIV-1의 외막 단백질인 gp120과의 상호작용을 저해하는 본 발명의 펩타이드는 그 크기가 화학적 합성이 가능한 수준으로 작으면서도 기존의 후천성 면역 결핍증 (acquired immunodeficiency syndrome, 이하 "AIDS"로 약칭함) 치료제의 작용 단계와는 전혀 다른 단계인 HIV-1 바이러스의 감염 초기 단계에 작용하여 세포 수용체인 CD4와 HIV-1의 � ��막 단백질인 gp120과의 상호작용을 특이적으로 저해하므로 새로운 AIDS 치료제로 개발될 수 있을 뿐만 아니라, 다른 AIDS 치료제와 병용되는 복합 치료 방법을 통하여 AIDS 치료에 효과적으로 사용될 수 있는 펩타이드이다. 또한, 본 발명에서는 아가로스 비드 (agarose bead)를 사용하는 특징적인 패닝방법을 사용하여 상기 펩타이드을 효과적으로 선별할 수 있다.
    • 2. 发明公开
    • 세포수용체와HIV의상호작용을저해하는항AIDS펩타이드
    • 抗艾滋病肽抑制细胞受体与人类免疫缺陷病毒(HIV)之间的相互作用
    • KR1020000021557A
    • 2000-04-25
    • KR1019980040708
    • 1998-09-30
    • 동화약품주식회사학교법인 포항공과대학교
    • 윤성준김종우성영철이경재신동혁김남두최요한박상진장환봉한진희
    • C07K7/08
    • C07K7/08C07K7/64
    • PURPOSE: Provided is a peptide inhibiting an interaction between gp120 that is outer membrane protein of HIV and a cell receptor, CD4 on a stage of cell infection of HIV CONSTITUTION: A peptide consists of 12 amino acids. each amino acid comprises especially, proline and phenylalanine on the fourth and sixth position from amino-ends respectively and random amino acids. Peptide inhibits interaction between cell receptor, CD4 and outer membrane of HIV-1, gp120 on an early step of virus infection so it can be provided as a new AIDS treatment and used for combination therapy. To select a peptide which can be used for AIDS therapy, panning method which is characterized by using agarose bead as matrix and phage-displayed peptide library, is provided. In the panning method, peptide is obtained by using phosphate-buffered saline, competitive binding, and E.coli used as a host cell of phage.
    • 目的:提供抑制HIV的外膜蛋白的gp120与细胞受体之间的相互作用的肽,HIV在细胞感染阶段的CD4组成:肽由12个氨基酸组成。 每个氨基酸分别特别包括氨基末端的第四和第六位上的脯氨酸和苯丙氨酸以及随机氨基酸。 肽在病毒感染的早期阶段抑制细胞受体,CD4和HIV-1外膜之间的相互作用,因此可以作为新的AIDS治疗提供并用于联合治疗。 为了选择可用于AIDS治疗的肽,提供以使用琼脂糖珠作为基质和噬菌体展示肽文库的淘选方法。 在淘选方法中,通过使用磷酸盐缓冲盐水,竞争性结合和用作噬菌体宿主细胞的大肠杆菌获得肽。
    • 3. 发明公开
    • 신규의 3-니트로피리딘 유도체 및 그를 포함하는 약학적조성물
    • 3-硝基吡啶衍生物和含有其的药物组合物
    • KR1020010061857A
    • 2001-07-07
    • KR1019990064403
    • 1999-12-29
    • 동화약품주식회사
    • 윤성준이상욱김남두박용균이근형김종우박상진
    • C07D213/72
    • PURPOSE: The 3-nitropyridine derivatives and a pharmaceutical composition containing the same are provided, which are useful for inhibiting the growth of hepatitis B virus(HBV) and human immunodeficiency virus(HIV). CONSTITUTION: The 3-nitropyridine derivatives are represented by formula (1), in which R1: is H; hydroxy; C2 to C6 dialkylamino; C2 to C6 linear or branched hydroxyalkyl; C3 to C6 linear or branched dihydroxyalkyl; C3 to C6 alkoxyalkyl; saturated or unsaturated hetero ring compound of 5 or 6 atoms that contains 1 to 3 hetero atoms selected from N, O or S and substituted or unsubstituted by C1 to C3 alkyl; and R1 contains as an asymmetric carbon, R2: is H; or C1 to C4 linear or branched alkyl, or R1 and R2 together form saturated membered hetero ring of 5 or 6 atoms, wherein the hetero ring contains 1 to 3 hetero atoms selected from N, O and S and substituted or unsubstituted by C1 to C5 linear or branched alkyl, C2 to C5 linear or branched hydroxyalkyl, or hydroxy, R3: is indazole-5-il or indazole-6-il, and n is an integer of 0 to 3. The pharmaceutical composition contains effective amounts of 3-nitropyridine derivatives.
    • 目的:提供3-硝基吡啶衍生物和含有它们的药物组合物,其可用于抑制乙型肝炎病毒(HBV)和人类免疫缺陷病毒(HIV)的生长。 构成:3-硝基吡啶衍生物由式(1)表示,其中R1:是H; 羟基; C2〜C6二烷基氨基; C2至C6直链或支链羟烷基; C3至C6直链或支链二羟基烷基; C3至C6烷氧基烷基; 含有1至3个选自N,O或S的杂原子并且被C1至C3烷基取代或未取代的5或6个原子的饱和或不饱和杂环化合物; R1含有不对称碳,R2为H; 或C1至C4直链或支链烷基,或R1和R2一起形成5或6个原子的饱和元杂环,其中该杂环含有1至3个选自N,O和S的杂原子并且被C1至C5取代或未取代 直链或支链烷基,C2至C5直链或支链羟烷基或羟基,R3为吲唑-5-基或吲唑-6-il,n为0至3的整数。该药物组合物含有有效量的3- 硝基吡啶衍生物。
    • 4. 发明公开
    • 신규의 5-피리미딘카르복스아미드 유도체 및 그를포함하는 약학적 조성물
    • 新的5-嘧啶甲酰胺衍生物和含有它的药物组合物
    • KR1020010048569A
    • 2001-06-15
    • KR1019990053294
    • 1999-11-27
    • 동화약품주식회사
    • 윤성준이상욱김남두박용균이근형김종우박상진박희정장환봉
    • C07D239/10
    • PURPOSE: Novel 5-pyrimidinecarboxamide derivatives inhibiting the growth of HBV and HIV, a pharmaceutically acceptable salt thereof, a preparation thereof and an antiviral composition containing the compound as an effective component are provided, which show less adverse effects and can be effectively used for prevention and treatment of HBV and HIV. CONSTITUTION: The novel 5-pyrimidinecarboxamide derivatives of formula 1 are prepared by the following processes: 4-chloro-2-methylthio-5-pyrimidinecarboxylic acid ethyl ester of formula 2 and 5-aminoindazole or 6-aminoindazole of the formula; R2-NH2 are reacted in the presence of a base to produce 5-pyrimidine carboxylic acid ethyl ester derivative of formula 4; and the obtained 5-pyrimidine carboxylic acid ethyl ester derivative is reacted with an amine compound(R1-NH2). In formula, R1 is H, C1-4 straight or branched alkyl, C3-6 cycloalkyl or C2-3 hydroxyalkyl; R2 is indazole-5-yl or indazole-6-yl.
    • 目的:提供抑制HBV和HIV生长的新型5-嘧啶甲酰胺衍生物,其药学上可接受的盐,其制备方法和含有该化合物作为有效成分的抗病毒组合物,其效果较差,可有效用于预防 以及治疗HBV和HIV。 构型:式1的新型5-嘧啶甲酰胺衍生物通过以下方法制备:式2的4-氯-2-甲硫基-5-嘧啶羧酸乙酯和下式的5-氨基吲唑或6-氨基吲唑; R2-NH2在碱的存在下反应,生成式4的5-嘧啶羧酸乙酯衍生物; 并将所得的5-嘧啶羧酸乙酯衍生物与胺化合物(R1-NH2)反应。 在式中,R 1是H,C 1-4直链或支链烷基,C 3-6环烷基或C 2-3羟基烷基; R2是吲唑-5-基或吲唑-6-基。
    • 8. 发明公开
    • 신규 2,5-피리딘디카복실산 유도체
    • 新的2,5-吡啶二羧酸
    • KR1020000031735A
    • 2000-06-05
    • KR1019980047918
    • 1998-11-10
    • 동화약품주식회사
    • 윤성준이상욱심형수박용균양왕용김종우박상진
    • C07D401/14
    • PURPOSE: 2,5-pyrimidinedicarboxylic acids and the method for manufacturing it are provided, which have effect on restraining the proliferation of HBV(Hepatitis B Virus) and HIV(Human Immunodeficiency Virus). CONSTITUTION: In the formula 1, R1 represents hydrogen, alkyl group, hydroxy alkyl group, alkoxy alkyl group, dihydroxy alkyl group and dialkoxy alkyl group and R2 represents hydrogen and alkyl group. 2,5-pyridinedicarboxylic acids(formula 1) can form organic or inorganic salt such as chloric acid, phosphoric acid, oxalic acid, maleic acid and tartaric acid which is admitted pharmaceutically. 2,5-pyridinedicarboxylic acids are prepared from following reaction(reaction 1). Piperazines are piperazine(R1=hydrogen), 1-methylpiperazine(R1=methyl group), 1-ethylpiperazine(R1=ethyl group), 1-(2-hydroxyethyl)piperazine(R1=2-hydroxyethyl group. Nicotinic acids(formula 2) are reacted with acyl chloride, product of this reaction is reacted with piperazine compounds and 2,5-pyrimidinedicarboxylic acids are prepared from this reaction.
    • 目的:提供2,5-嘧啶二羧酸及其制备方法,其具有抑制HBV(乙型肝炎病毒)和HIV(人类免疫缺陷病毒)增殖的作用。 构成:在式1中,R 1表示氢,烷基,羟基烷基,烷氧基烷基,二羟基烷基和二烷氧基烷基,R 2表示氢和烷基。 2,5-吡啶二羧酸(式1)可以形成有机或无机盐,例如药学上允许的氯酸,磷酸,草酸,马来酸和酒石酸。 从以下反应制备2,5-吡啶二羧酸(反应1)。 哌嗪是哌嗪(R1 =氢),1-甲基哌嗪(R1 =甲基),1-乙基哌嗪(R1 =乙基),1-(2-羟乙基)哌嗪(R1 = 2-羟乙基)烟酸(式2 )与酰氯反应,将该反应产物与哌嗪化合物反应,并从该反应制备2,5-嘧啶二羧酸。
    • 10. 发明公开
    • 항바이러스제로 유용한 6-메틸니코틴아미드 유도체
    • 用作抗病毒剂的6-甲基二酰胺衍生物
    • KR1020010096176A
    • 2001-11-07
    • KR1020000020137
    • 2000-04-17
    • 동화약품주식회사
    • 윤성준이상욱이진수김남두이근형이학동김종우박상진박희정
    • C07D417/06
    • PURPOSE: 6-methylnicotineamide derivatives useful as antiviral agents are provided, thereby inhibiting the growth of hepatitis B virus(HBV), hepatitis C virus(HCV) and human immunodeficiency virus(HIV). CONSTITUTION: The 6-methylnicotineamide derivatives are represented by formula(1), in which R1 is hydroxy, C1 to C5 linear or branched alkyl, C3 to C6 cyclo alkyl, C2 to C6 dialkylamino, or saturated or unsaturated hetero ring having 5 or 6 atoms, in which the hetero ring comprises 1 to 2 hetero atoms selected from N, O or S, and unsubstituted or substituted with C1 to C3 alkyl; and m is an integer of 0 or 1; R2 is hydrogen or C1 to C4 alkyl; or both R1 and R2 form hetero ring having 5 to 6 atoms, in which the hetero ring comprises 1 to 2 hetero atoms selected from N, O or S; and n is an integer of 0 to 4.
    • 目的:提供用作抗病毒药物的6-甲基烟酰胺衍生物,从而抑制乙型肝炎病毒(HBV),丙型肝炎病毒(HCV)和人类免疫缺陷病毒(HIV)的生长。 构成:6-甲基烟酰胺衍生物由式(1)表示,其中R1是羟基,C1至C5直链或支链烷基,C3至C6环烷基,C2至C6二烷基氨基或饱和或不饱和杂环,具有5或6 原子,其中杂环包含1至2个选自N,O或S的杂原子,未取代或被C 1至C 3烷基取代; m为0或1的整数; R2是氢或C1-C4烷基; 或者R 1和R 2都形成具有5至6个原子的杂环,其中杂环包含1至2个选自N,O或S的杂原子; n为0〜4的整数。